2-(1,3-benzothiazol-2-yl)-4-[(4-fluorophenyl)thio]-5-methyl-3-pyrazolamine, also known as **BZT**, is a compound with potential pharmacological activity. Its importance lies in its potential applications as a:
**1. Anticancer Agent:**
* **BZT has shown promising anticancer activity in preclinical studies.** Its mechanism of action is believed to be through inhibition of the enzyme **topoisomerase I**, which is crucial for DNA replication and cell division.
* **Targeting topoisomerase I can lead to DNA damage and ultimately cell death, effectively inhibiting tumor growth.**
**2. Antibacterial Agent:**
* **BZT has also demonstrated antibacterial activity against certain bacteria, including Staphylococcus aureus.**
* **This is likely due to its ability to disrupt bacterial cell wall synthesis.**
**3. Anti-inflammatory Agent:**
* **Research suggests that BZT might possess anti-inflammatory properties.** This is based on its potential to inhibit the production of pro-inflammatory cytokines.
**Current Research Focus:**
Current research on BZT mainly focuses on:
* **Determining its exact mechanism of action.**
* **Investigating its efficacy and safety in preclinical models.**
* **Exploring its potential for clinical development as a therapeutic agent for cancer, bacterial infections, or inflammatory conditions.**
**Why is it important for research?**
BZT is a promising candidate for drug development due to its multi-faceted biological activity. Its potential to be effective against a range of diseases, including cancer, bacterial infections, and inflammatory conditions, makes it an important subject of ongoing research.
**Note:**
It's important to emphasize that BZT is still in the early stages of research and has not yet been approved for any medical use.
ID Source | ID |
---|---|
PubMed CID | 2320295 |
CHEMBL ID | 1595499 |
CHEBI ID | 121330 |
Synonym |
---|
MLS000055024 |
smr000065831 |
CHEBI:121330 |
ZINC03190290 |
2-(1,3-benzothiazol-2-yl)-4-(4-fluorophenyl)sulfanyl-5-methylpyrazol-3-amine |
HMS2485J20 |
CHEMBL1595499 |
2-(1,3-benzothiazol-2-yl)-4-[(4-fluorophenyl)thio]-5-methyl-3-pyrazolamine |
Q27209866 |
Z56788273 |
Class | Description |
---|---|
aryl sulfide | Any organic sulfide in which the sulfur is attached to at least one aromatic group. |
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res] |
Protein | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
---|---|---|---|---|---|---|---|
Chain A, Cruzipain | Trypanosoma cruzi | Potency | 12.5893 | 0.0020 | 14.6779 | 39.8107 | AID1476 |
Luciferase | Photinus pyralis (common eastern firefly) | Potency | 1.6944 | 0.0072 | 15.7588 | 89.3584 | AID588342 |
BRCA1 | Homo sapiens (human) | Potency | 2.2387 | 0.8913 | 7.7225 | 25.1189 | AID624202 |
ATAD5 protein, partial | Homo sapiens (human) | Potency | 6.2406 | 0.0041 | 10.8903 | 31.5287 | AID504466; AID504467 |
TDP1 protein | Homo sapiens (human) | Potency | 12.2798 | 0.0008 | 11.3822 | 44.6684 | AID686978; AID686979 |
PINK1 | Homo sapiens (human) | Potency | 10.0000 | 2.8184 | 18.8959 | 44.6684 | AID624263 |
Parkin | Homo sapiens (human) | Potency | 10.0000 | 0.8199 | 14.8306 | 44.6684 | AID624263 |
P53 | Homo sapiens (human) | Potency | 70.7946 | 0.0731 | 9.6858 | 31.6228 | AID504706 |
NPC intracellular cholesterol transporter 1 precursor | Homo sapiens (human) | Potency | 3.1623 | 0.0126 | 2.4518 | 25.0177 | AID485313 |
nuclear factor erythroid 2-related factor 2 isoform 2 | Homo sapiens (human) | Potency | 7.3078 | 0.0041 | 9.9848 | 25.9290 | AID504444 |
ras-related protein Rab-9A | Homo sapiens (human) | Potency | 1.1220 | 0.0002 | 2.6215 | 31.4954 | AID485297 |
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] |
Assay ID | Title | Year | Journal | Article |
---|---|---|---|---|
AID1745845 | Primary qHTS for Inhibitors of ATXN expression | |||
AID588497 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set | 2010 | Current protocols in cytometry, Oct, Volume: Chapter 13 | Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening. |
AID588497 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set | 2006 | Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5 | Microsphere-based protease assays and screening application for lethal factor and factor Xa. |
AID588497 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set | 2010 | Assay and drug development technologies, Feb, Volume: 8, Issue:1 | High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors. |
AID588499 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set | 2010 | Current protocols in cytometry, Oct, Volume: Chapter 13 | Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening. |
AID588499 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set | 2006 | Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5 | Microsphere-based protease assays and screening application for lethal factor and factor Xa. |
AID588499 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set | 2010 | Assay and drug development technologies, Feb, Volume: 8, Issue:1 | High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors. |
AID504810 | Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign | 2010 | Endocrinology, Jul, Volume: 151, Issue:7 | A small molecule inverse agonist for the human thyroid-stimulating hormone receptor. |
AID588501 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set | 2010 | Current protocols in cytometry, Oct, Volume: Chapter 13 | Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening. |
AID588501 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set | 2006 | Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5 | Microsphere-based protease assays and screening application for lethal factor and factor Xa. |
AID588501 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set | 2010 | Assay and drug development technologies, Feb, Volume: 8, Issue:1 | High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors. |
AID651635 | Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression | |||
AID504812 | Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign | 2010 | Endocrinology, Jul, Volume: 151, Issue:7 | A small molecule inverse agonist for the human thyroid-stimulating hormone receptor. |
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |
Timeframe | Studies, This Drug (%) | All Drugs % |
---|---|---|
pre-1990 | 0 (0.00) | 18.7374 |
1990's | 0 (0.00) | 18.2507 |
2000's | 1 (20.00) | 29.6817 |
2010's | 3 (60.00) | 24.3611 |
2020's | 1 (20.00) | 2.80 |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |
According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be weak demand-to-supply ratio for research on this compound.
| This Compound (12.56) All Compounds (24.57) |
Publication Type | This drug (%) | All Drugs (%) |
---|---|---|
Trials | 0 (0.00%) | 5.53% |
Reviews | 0 (0.00%) | 6.00% |
Case Studies | 0 (0.00%) | 4.05% |
Observational | 0 (0.00%) | 0.25% |
Other | 5 (100.00%) | 84.16% |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |